Pharmacology Week 7-9 Flashcards
1
Q
2 main divisions of autonomic nervous system
A
- sympathetic
- parasympathetic
2
Q
link between the CNS and peripheral organs
A
autonomic nervous system
3
Q
What does the autonomic nervous system help regulate?
A
- contraction and relaxation of vascular and visceral smooth muscle
- all exocrine and certain endocrine secretions
- the heartbeat
-energy metabolism(
liver and skeletal muscle)
4
Q
what autonomic nervous system is closer to the end organ?
A
Parasympathetic “rest and digest”
5
Q
- active in resting phase
- conserves energy
- Acetylcholine ONLY
A
parasympathetic
6
Q
- fight or flight
- energy expenditure
- both acetylcholine and noradrenaline
A
sympathetic
7
Q
What does parasympathetic nervous system do?
A
- constricts pupils
- stimulate saliva
- slo heartbeat
- constrict airways
- stimulate activity of stomach
- inhibit release of glucose, stimulates gallbladder
- stimulate activity of intestine
- contracts bladder
- promote erection of genitals
8
Q
What does sympathetic nervous system do?
A
- dilate pupils
- stimulate saliva
- increase heartbeat
- relax airways
- inhibit activity of stomach
- stimulate release of glucose, inhibits gallbladder
- inhibit activity of intestine
- secrete epinephrine and norepinephrine
- relax bladder
- promote ejaculation and vaginal contraction
9
Q
All preganglionic nerve fibers are myelinated and release ______ from the nerve terminals
A
ACh
10
Q
ACh produces excitatory postsynaptic potential in postganglionic neurons by activating ___________
A
nicotinic receptors
11
Q
sympathetic postganglionic releases mainly__________
A
noradrenaline
12
Q
parasympathetic postganglionic releases mainly__________
A
acetylcholine
13
Q
what receptors are used for parasympathetic nervous system?
A
cholinergic receptors
14
Q
What are the cholinergic receptors?
A
Muscarinic receptors
nicotinic
15
Q
M1:
M2:
M3:
A
- CNS and gastric parietal cells
- heart
- smooth muscle and glands
16
Q
motor end plate, autonomic ganglia and adrenal medulla (targets)
A
nicotinic receptors
17
Q
indications for local anesthetics:
A
- infiltration, nerve block, epidural and intrathecal anesthesia
- topical anaesthesia
18
Q
lidocaine, benzocaine, prilocaine, cocaine examples of…..
A
local anesthetics
19
Q
block impulse propagation and abolish sensations in a limited area
A
local anesthetics
20
Q
What is the mechanism of action for local anesthetics?
A
- blocking sodium channels in nerve membrane
- drugs raise electrical excitation threshold (thus no action potential)
- eventually slow and blocks the propagation
21
Q
What are the sympathetic nervous system receptors called?
A
adenoceptors
22
Q
different types of adenoreceptors?
A
- alpha 1 (postsynaptic)
- alpha 2 (presynaptic)
- beta 1
- beta 2
23
Q
What is the different b/w beta 1 and 2 receptors?
A
- beta 1: heart
- beta 2: bronchial (lungs)
24
Q
describe the cholinergic junction (acetylcholine synthesis, release and signal breakdown)
A
1) acetylcholine is formed
2) packaged up in vesicles to lean the axon
3) released and crosses the synapse
4) binds to receptor activating a signalling cascade
5) cleared from synapse by acetylcholinesterase
25
acetylcholine is formed by an enzyme:
| ___________ + __________
Acetyl CoA + Choline
26
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activates muscarinic receptors, producing excitatory effects such as
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muscarinic agonists
- miosis
- sweating/ salivation
- decrease in heart rate
- bronchial constriction
- increased GI motility/ relaxation of sphincters
27
if you block agonist receptors what would the effects be?
called an antagonist and the effects would be the inverse
28
neostigmine (myasthenia gravis) and donepezil (alzheimers)
anticholinesterases
29
breaks down acetylcholine
anticholinesterases
30
anticholinergics/ antimuscarinics
cholinergic receptors antagonists
31
- not clinically useful for ANS (ganglion blockers)
| - muscle relaxants act on the neuromuscular junction
nACh receptors antagonists
32
-parasympatholytic, antimuscarinic or anticholinergic drugs because they compete and block the action of Each at the muscarinic receptors
mACh receptor antagonists
33
adenoceptor agonists
sympathomimetics
34
main effects of receptor activation...
-alpha 1 receptors:
- alpha 2 receptors
- beta 1 receptors:
- beta 2 receptors:
- vasoconstriction
- inhibition of transmitter release
- increased cardiac rate and force (beta 1)
- bronchodilation (beta 2)
35
asthma relievers (salbutamol) example of what type of sympathomimetics?
beta 2-adenoceptor agonist
36
adrenaline (EpiPen) example of what type of sympathomimetics?
alpha/ beta adenoceptor agonist
37
decongestants are example of what type of sympathomimetics?
alpha 1- adenoceptor agonist
38
drugs affecting the somatic nervous system?
botulinum toxins
39
drugs inhibiting acetylcholine release
presynaptic agents
40
inhibits the reuptake of noradrenaline (block NET)
stimulants (cocaine, amphetamines-used in ADHD)
41
increases noradrenaline release
stimulants
| amphetamines-used in ADHD
42
blockers usually have the suffix ____
-lol
43
adrenoceptor antagonist examples
- non selective beta blockers ( blocks beta 1 and 2)
- selective beta 1 blocker (cardioselective)
- non-selective beta-blockers (blocks alpha or beta)
44
how many deaths were due to cardiovascular disease (in 2017)
1 in 4
45
treatment of systemic hypertension, cardiac failure, shock, peripheral vascular disease, Raynaud's disease and pulmonary hypertension
vasoactive drugs
46
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drugs that act on the heart are used for
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-arrhythmias
-cardiac failure
-hypertension
-coronary insufficiency
(myocardial infarction and angina)
47
non-pharmacological management for hypertension:
- lifestyle:
- absolute risk:
- lifestyle (exercise, smoking, cessation, diet, weight loss)
- probability of cardiovascular event w/in 5 years), high cholesterol, diabetes, being obese/inactive
48
management of hypertension (drug classes)
- ACE inhibitor or angiotensin II receptor antagonist
- calcium channel blocker
- low-dose thiazide diuretic
49
examples) captopril, Enalapril, ramipril
ACE inhibitors
50
How do ACE inhibitors work?
- low Na concentration juxtaglomerular cells secrete renin
- goes into blood and angiotensin I is formed
- angiotensin-converting enzyme in pulmonary blood (ACE) forms angiotensin II (which is what is blocked in ACE inhibitors)
- causes vasoconstriction or aldosterone
51
what happens if there is not enough angiotensin II?
- decreased vasoconstriction; more vasodilation
| - less resistant ; decreased blood pressure
52
What does aldosterone stimulate?
stimulates sodium uptake on the cell
53
What is the mechanism of action for ACE inhibitors?
blocks conversion of angiotensin I to angiotensin II
also inhibits breakdown of bradykinin
54
what's ACE stand for?
angiotensin converting enzyme
55
what are the adverse effects of ACE inhibitors?
-non productive cough (due to increase in bradykinin)
56
what are the main contraindications for ACE inhibitors??
pregnancy and renal failure
57
What are the main drug interactions with ACE inhibitors?
- loop diuretics
- NSAIDs
- sartans
*all affect kidneys*
58
examples: candesartan, irbesartan, telmisartan
sartans: angiotensin receptor blocker
doesn't block enzyme- blocks receptor
59
What part of the pathway is broken down in tartan use for angiotensin?
- low Na concentration juxtaglomerular cells secrete renin
- goes into blood and angiotensin I is formed
- angiotensin-converting enzyme in pulmonary blood (ACE) forms angiotensin II
- (this part is blocked in sartans) causes vasoconstriction or aldosterone
60
What is the mechanism of action for angiotensin receptor blockers (ARB)
competitive antagonist to type 1 angiotensin receptors
61
what is a common adverse effect for ARB's?
myalgia
62
examples: dihydropyridine (-dipine) and non-dihydropyridine (verapamil and diltiazem)
calcium channel blockers
63
What is the mechanism of action for calcium channel blockers?
reduce calcium entry into cells of myocardium, vascular smooth muscle, and cardiac conducting system by preventing L-type calcium channels from opening
64
What are the adverse effects of calcium channel blockers?
- flushing
| - peripheral edema --> are usually prescribed diuretics but in this case they won't work. (dihydropyridines)
65
example: hydrochlorothiazide (HCT)
thiazide diuretics
66
What is the mechanism of action for thiazide diuretics?
inhibits reabsorption of sodium and chloride in the proximal (diluting) segment of the distal convoluted time
-low doses --> vasodilator effect
67
what are adverse effects to thiazide diuretics?
-weakness, muscle cramps
68
What are contraindications for thiazide diuretics?
- gout (can affects excretion of uric acid)
| - diabetes
69
suffix -lol
beta blockers
70
what is the mechanism of action for beta blockers?
- competitive antagonist of the beta- adrenergic receptor, decreasing HR, BP, and cardiac contractility
- decrease renin production
71
What are drugs used for heart failure?
- ACE inhibitors, ARB
- beta- blockers
- loop diuretic (edema)
72
Why are ACE inhibitors and ARB the first line therapy with beta blockers for heart failure?
the reduction in vascular tone decreased the work and oxygen demand of the failing heart
73
increase the excretion of sodium and water useful for hypertension, HF, renal failure, nephrotic syndrome and cirrhosis
diuretics
74
example: furosemide
loop diuretic
75
What is the mechanism of action for loop diuretics?
- potent diuretic (water tablets)
- inhibit reabsorption of sodium and chloride in the ascending limb of the loop of Henle (inhibits Na/K)
- fast and intense diuresis
76
What are interaction with other drugs and loop diuretics?
- drugs that cause hypokalaemia
| - NSAIDs
77
What are common adverse reaction for drugs used for arrhythmias?
potential to worsen the arrhythmia
78
"white clots" platelet rich
arterial
79
"red clots"
| RBC and fibrin
venous
80
inactivates coagulation process and inhibits development of clots
anticoagulants
81
Vitamin K antagonists (anticoagulants)
Warfarin (Coumadin, Marevan)
82
Factor Xa inhibitor (anticoagulant)
Aprixaban (eliquis) and rivaroxaban (xarelto)
83
Direct thrombin inhibitors (anticoagulants)
dabigatran (Pradaxa)
84
inhibits synthesis of Vitamin k dependent clotting factors (II, VII, IX, X) and antithrombotic factos protein C and S
warfarin
85
What is a common adverse effect of warfarin
bleeding
86
reversibly inhibits both free and fibrin-bound thrombin, preventing conversion of fibrinogen to fibrin, preventing thrombus formation
dabigatran
87
What are adverse effects of dabigatran?
bleeding and gastritis/ dyspepsia
88
(directly affects the cascade) selectively inhibits factor Xa, blocking thrombin to fibrin and thrombus development
rivaroxaban and apixaban
89
Where do heparins work?
directly inhibit antithrombin part of cascade
90
Where does dabigatran work?
directly inhibits thrombin IIa
91
used in the management of arterial thrombosis (clots initially made of platelets) but not VTE (fibrin clots)
antiplatelets
92
examples of anti platelets
aspirin (low dose)
clopidogrel (plavix)
93
inhibits platelet aggregation by irreversibly inhibiting COX, reducing the synthesis of thrombin A2
aspirin
94
What are common adverse effects of aspirin
GI irritation
| asymptotic blood loss and increased bleeding time
95
irreversibly binds to the platelet P2Y12 receptor and inhibits the platelet aggregation for the life of the platelet
clopidogrel
96
improving the balance between myocardial oxygen supply and demand
antiangiinal drugs
- Beta blockers
- calcium channel blockers
- nitrates (short/long acting)
97
What is usually the first line therapy for stable angina?
beta 1- blockers
98
glyceryl trinitrate, isosorbide denigrate, isosorbide mononitrate
- shot acting nitrate
| - long acting nitrates
99
mediates vasodilation
| -by reducing myocardium oxygen required by reducing venous return and preload to the heart
nitrates
100
adverse effects of erythropoietin agonists
- myalgia
- hypertension
- bone pain
- headaches
- peripheral oedema
101
recombinant glycoprotein which binds to erythropoietin receptors and stimulates erythropoiesis (doping)
erythropoietin agonists
102
drugs used in anaemia
folic acid, B12, iron, erythropoietin agonists
103
required for synthesis of purine and pyrimidine bases (DNA) and for amino acid metabolism and normal erythropoiesis
folic acid
104
adverse effects of folic acid
- rash
- sleep disturbance
- no common adverse effects
105
essencial for nerve development, unclean acid synthesis and normal erythropoiesis (necessary for absorption)
B12
106
required for the formation of hemoglobin and myoglobin
iron
107
common adverse effects of iron
-abdominal pain
=nausea
-vomiting
-constipation **
108
what does erythropoiesis require?
- iron
- vitamin B12
- folic acid
- erythropoietin agonists
109
What were the top 3 drugs prescribed in 2018?
1) rosuvastatin
2) atorvastatin
3) esomeprazole
110
human monoclonal antibody and increases the number of LDL receptors by inhibiting their degradation by PCSK9 (evolocumab, alirocumab)
PCSK9 inhibitor
111
what does PCSK9 inhibitor effect?
significantly decreases LDL- concentration
112
ezetimibe
-blocks cholesterol transport protein in intestinal wall, without affecting the absorption of fat-soluble vitamins, bile acids, triglycerides
Cholesterol absorption inhibitor
-usually prescribed with statins (adverse effects common)
113
What are the lipid lowering drugs?
- HMG-CoA reductase inhibitors (statins)
- cholesterol absorption inhibitors
- PCSK9 inhibitors
114
atorvastatin, fluvastatin, pravastatin, rosuvastatin, simvastatin
HMG-CoA reductase inhibitors (statins)
115
limiting enzyme in cholesterol synthesis
HMG-CoA reductase
116
what are indications for statin use?
- high risk of coronary heart disease
| - hypercholesterolaemia
117
abnormal amounts of lipid in the blood
-lipoproteins are synthesized by _____
cholesterol
-liver
